Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

C. M. van Esbroeck, Annelot; P. A. Janssen, Antonius; B. Cognetta, Armand; Ogasawara, Daisuke; Shpak, Guy; van der Kroeg, Mark; Kantae, Vasudev; P. Baggelaar, Marc; M. S. de Vrij, Femke; Deng, Hui; Allarà, Marco; Fezza, Filomena; Lin, Zhanmin; van der Wel, Tom; Soethoudt, Marjolein; D. Mock, Elliot; den Dulk, Hans; L. Baak, Ilse; I. Florea, Bogdan; Hendriks, Giel; De Petrocellis, Luciano; S. Overkleeft, Herman; Hankemeier, Thomas; I. De Zeeuw, Chris; Di Marzo, Vincenzo; Maccarrone, Mauro; F. Cravatt, Benjamin; A. Kushner, Steven; van der Stelt, Mario

doi:10.1126/science.aaf7497

Public

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

Shared by NobleBlocks on Jun 9, 2017 • 12:00 AM UTC

Authors:

Annelot C. M. van Esbroeck

Antonius P. A. Janssen

Armand B. Cognetta

Abstract

A clue to a drug's neurotoxicity? The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as a potential treatment for anxiety and pain. In a phase 1 trial of the drug, one subj...

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